Influence of rifampicin treatment on antipyrine clearance and metabolite formation in patients with tuberculosis.

Teunissen, MW; Bakker, Willem H.; Meerburg‐Torren, JE Van der; Breimer, D.D.

doi:10.1111/j.1365-2125.1984.tb02532.x

Cited by 28 publications

(14 citation statements)

References 31 publications

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“…After RIM the rate of formation, expressed as clearance for production (17), of NORA, OHA and HMA increased by 177, 91, and 70%, respectively, whereas only the clearance for production of NORA was significantly increased by 53% after RIB. These results are in reasonable agreement with those reported in previous studies (17,18), in which RIM was shown to preferentially stimulate the formation of NORA in humans. This is in contrast to phenytoin and carbamazepine which mostly enhance the formation of OHA, to a lesser degree that of HMA, and have no effect on the NORA pathway (19).…”

Section: Inducton Properties Of Rifampicin and Rifabutin In Animalssupporting

confidence: 83%

Induction and autoinduction properties of rifamycin derivatives: a review of animal and human studies.

Benedetti¹,

Dostert²

1994

Environ Health Perspect

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Animal studies have demonstrated that the mouse and rabbit are far more responsive to the inductive properties of rifamycin derivatives than the rat and guinea pig. The rat hepatic cytochrome P450 system seems to be resistant to the action of rifampicin unless very high doses are used. Mouse hepatic microsomal mixed-function oxidase activity is markedly increased by repeated dosing with rifampicin, whereas administration of rifabutin may be ineffective. In humans, both rifampicin and rifabutin are extensively metabolized and induce their own metabolism. The induced metabolic pathways remain essentially unknown. Under autoinduction conditions, the elimination half-life of rifampicin decreases, whereas that of rifabutin is not altered. Although the effects of repeated administration of rifampicin and rifabutin on the various forms of cytochrome P450 in humans have not been extensively examined, there is convincing evidence that the P4503A subfamily is induced by either drug, whereas the P4501 A subfamily and P4502D6 do not appear to be affected by rifampicin. Limited reliable information is available concerning the induction of human glucuronyltransferase activities by rifampicin and rifabutin which, however, do not seem to influence zidovudine glucuronide formation in healthy subjects.

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Section: Inducton Properties Of Rifampicin and Rifabutin In Animalssupporting

confidence: 83%

Induction and autoinduction properties of rifamycin derivatives: a review of animal and human studies.

Benedetti¹,

Dostert²

1994

Environ Health Perspect

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“…In agreement with previous reports on rifampicin (Miguet et al, 1977;Toverud et al, 1981;Bennett et al, 1982) Teunissen et al, 1984), subjects with lower initial values for antipyrine clearance tended to be more inducible than those with higher values. Twelve days after stopping rifapentine, antipyrine t,½, still showed a small but significant decrease, consistent with the relatively slow turnover of induced monooxygenase activity in man .…”

Section: Discussionsupporting

confidence: 82%

Induction of mixed function oxidase activity in man by rifapentine (MDL 473), a long‐acting rifamycin derivative.

Durand¹,

Hampden²,

Boobis³

et al. 1986

Brit J Clinical Pharma

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The effects of rifapentine (MDL 473) administration on hepatic mixed function oxidase activity in man have been investigated in six healthy volunteers. Administration of rifapentine (600 mg 48 h‐1) for 10 days resulted in a significant reduction in antipyrine half‐life (from 13.2 +/‐ 1.0 h to 7.7 +/‐ 0.4 h) and a corresponding increase in its total body clearance (from 41.8 +/‐ 5.5 ml min‐1 to 67.4 +/‐ 5.6 ml min‐1). Twelve days after stopping rifapentine administration, these values had largely returned to base‐line. 24‐Hour excretion of 6 beta‐ hydroxycortisol was significantly increased, by approximately three‐ fold, following administration of rifapentine for 10 days. Again, 12 days after stopping drug administration, 6 beta‐hydroxycortisol excretion had returned to pretreatment values. Clearance of antipyrine to its three oxidative metabolites was increased by rifapentine administration, although the increase for 3‐hydroxymethylantipyrine was not significant. The greatest increase (+140%) was observed for norantipyrine. Twelve days after the last dose of rifapentine, all values had returned to control levels. It is concluded that, like rifampicin, rifapentine is a potent inducer of mixed function oxidase activity in man and that the possibility of clinically significant drug interactions should be anticipated in the therapeutic use of this compound.

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“…Conversely, the rate of formation of NORA was reduced more than that of OHA or HMA in patients with alcoholic cirrhosis (Teunissen et al, 1984b). Thus, Ndemethylation reactions may be more readily affected in either direction than hydroxylations.…”

Section: Resultsmentioning

confidence: 90%

The disposition of antipyrine and its metabolites in young and elderly healthy volunteers.

Posner

Danhof

Teunissen

et al. 1987

Brit J Clinical Pharma

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1 Oxidative metabolism of antipyrine (AP) was compared in 11 elderly (> 65 years) and 12 young (< 40 years) volunteers. All subjects were non-smokers, consumed little if any alcohol and were in good health. 2 After a single dose of AP 500 mg, its clearance from saliva and profiles of the parent drug and its major metabolites in urine were determined using high-performance liquid chromatography. 3 Mean total AP clearance from saliva was lower in the elderly (P < 0.05). Mean weightnormalised volume of distribution was also smaller (P < 0.01) so that elimination half-life in the elderly was not significantly different from that in the young. 4 The percentage dose excreted in 48 h urine as norantipyrine (NORA) and its clearance for production were lower in the elderly (P < 0.001 and P < 0.01 respectively). Urinary 3-hydroxymethylantipyrine (HMA) and free antipyrine were present in greater quantities in 48 h urine in the elderly (P < 0.001 and P < 0.05) while the amounts of 4-hydroxyantipyrine (OHA) were almost identical in the two age groups. 5 The findings suggest that there is a selective impairment of N-demethylation in the elderly which may have important implications for dosage of elderly patients with drugs metabolised by this route.

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Influence of rifampicin treatment on antipyrine clearance and metabolite formation in patients with tuberculosis.

Cited by 28 publications

References 31 publications

Induction and autoinduction properties of rifamycin derivatives: a review of animal and human studies.

Induction and autoinduction properties of rifamycin derivatives: a review of animal and human studies.

Induction of mixed function oxidase activity in man by rifapentine (MDL 473), a long‐acting rifamycin derivative.

The disposition of antipyrine and its metabolites in young and elderly healthy volunteers.

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